Minicapsules encapsulating nanoparticles for targeting, apoptosis induction and treatment of colon cancer

Figures & data

Figure 1. Transmission electron microscopy of U-CH NP (A), (B) U-FA-CH NP, (C) atomic force microscopy of U-CH NP and (D) U-FA-CH NP.

Table1. Particle size, zeta potential and entrapment efficiency (EE %) of U-CH-NP and U-FA-CH-NP.

S.no	Formulation code	Particle size(nm)^a	Zeta Potential	EE (%)^a
1	U-CH NP	156 ± 5.3	+24.3 ± 1.4 mV	53.2 ± 1.2
2	U-FA-CH NP	240 ± 3.5	+16.3 ± 2.2 mV	62.1 ± 1.5

^aValues represent mean ± S.D (n = 6).

Figure 2. (A) Caspase 3 colorimetric assay. Significant differences were observed as compared to control (*p < .01), (B) percentage of cells in various phases of cell cycle 2 h and 12 h post treatment, (C) DNA Cell cycle analysis, Cells (in percentage) at G1, S, G2 phases of cell cycle and apoptosis at 2h and 12 h post-treatment, and (D) percentage cell viability of different formulations in Caco-2 cells.

Table 2. IC₅₀ Values of different formulation on Caco-2 cells.

IC50
Free UCN 01	U-CH-NP	U-FA-CH NP
0.13 ± 0.02	0.29 ± 0.005	0.16 ± 0.009

Figure 3. In Vivo distribution profiles of various formulations at different time intervals. (A) Tumor drug concentrations after oral administration of different formulations, (B) effect of free UCN 01 and various nanoparticle formulations on tumor growth in mice as compared to control, (C) Kaplan–Meir survival plot, (D) histopathology of stomach, small intestine and colon 10 h after formulation administration and (E) stability assessment of U-CH NP and U-FA-CH NP.

Table 3. Tumor distribution profile.

Pharmacokinetic parameter/ Formulations	t1/2 (h)	AUC0–∞ (µg h/mL)	MRT (h)	AUMC0–∞ (µg h^2/mL)
UCN 01^^	1.97 ± 0.25	53.39 ± 7.60	6.46 ± 0.03	346.50 ± 16.03
E-U-CH NP	6.29 ± 1.87**	484.81 ± 8.22¥	18.48 ± 1.24¥	8959.29 ± 151.90#
E-U-FA CH NP	9.81 ± 2.01¥	823.68 ± 6.32#	23.61 ± 1.75#	19,659.57 ± 1228.95#

**p < .05; ¥p < .01; #p < .001 compared to UCN 01^{^} group.